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| Title : Optimization of Activity, Selectivity, and Liability Profiles in 5-Oxopyrrolopyridine DPP4 Inhibitors Leading to Clinical Candidate (Sa)-2-(3-(Aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b]py ridin-6(7H)-yl)-N,N-dimethylacetamide (BMS-767778) - Devasthale_2013_J.Med.Chem_56_7343 |
| Author(s) : Devasthale P , Wang Y , Wang W , Fevig J , Feng J , Wang A , Harrity T , Egan D , Morgan N , Cap M , Fura A , Klei HE , Kish K , Weigelt C , Sun L , Levesque P , Moulin F , Li YX , Zahler R , Kirby MS , Hamann LG |
| Ref : Journal of Medicinal Chemistry , 56 :7343 , 2013 |
| Abstract : Devasthale_2013_J.Med.Chem_56_7343 |
| ESTHER : Devasthale_2013_J.Med.Chem_56_7343 |
| PubMedSearch : Devasthale_2013_J.Med.Chem_56_7343 |
| PubMedID: 23964740 |
| Gene_locus related to this paper: human-DPP4 |
| Title : 7-Oxopyrrolopyridine-derived DPP4 inhibitors-mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site - Wang_2011_Bioorg.Med.Chem.Lett_21_6646 |
| Author(s) : Wang W , Devasthale P , Wang A , Harrity T , Egan D , Morgan N , Cap M , Fura A , Klei HE , Kish K , Weigelt C , Sun L , Levesque P , Li YX , Zahler R , Kirby MS , Hamann LG |
| Ref : Bioorganic & Medicinal Chemistry Lett , 21 :6646 , 2011 |
| Abstract : Wang_2011_Bioorg.Med.Chem.Lett_21_6646 |
| ESTHER : Wang_2011_Bioorg.Med.Chem.Lett_21_6646 |
| PubMedSearch : Wang_2011_Bioorg.Med.Chem.Lett_21_6646 |
| PubMedID: 21996520 |
| Gene_locus related to this paper: human-DPP4 |
| Title : Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes - Augeri_2005_J.Med.Chem_48_5025 |
| Author(s) : Augeri DJ , Robl JA , Betebenner DA , Magnin DR , Khanna A , Robertson JG , Wang A , Simpkins LM , Taunk P , Huang Q , Han SP , Abboa-Offei B , Cap M , Xin L , Tao L , Tozzo E , Welzel GE , Egan DM , Marcinkeviciene J , Chang SY , Biller SA , Kirby MS , Parker RA , Hamann LG |
| Ref : Journal of Medicinal Chemistry , 48 :5025 , 2005 |
| Abstract : Augeri_2005_J.Med.Chem_48_5025 |
| ESTHER : Augeri_2005_J.Med.Chem_48_5025 |
| PubMedSearch : Augeri_2005_J.Med.Chem_48_5025 |
| PubMedID: 16033281 |
| Title : Synthesis of novel potent dipeptidyl peptidase IV inhibitors with enhanced chemical stability: interplay between the N-terminal amino acid alkyl side chain and the cyclopropyl group of alpha-aminoacyl-l-cis-4,5-methanoprolinenitrile-based inhibitors - Magnin_2004_J.Med.Chem_47_2587 |
| Author(s) : Magnin DR , Robl JA , Sulsky RB , Augeri DJ , Huang Y , Simpkins LM , Taunk PC , Betebenner DA , Robertson JG , Abboa-Offei BE , Wang A , Cap M , Xin L , Tao L , Sitkoff DF , Malley MF , Gougoutas JZ , Khanna A , Huang Q , Han SP , Parker RA , Hamann LG |
| Ref : Journal of Medicinal Chemistry , 47 :2587 , 2004 |
| Abstract : Magnin_2004_J.Med.Chem_47_2587 |
| ESTHER : Magnin_2004_J.Med.Chem_47_2587 |
| PubMedSearch : Magnin_2004_J.Med.Chem_47_2587 |
| PubMedID: 15115400 |